摘要
达那唑(Danazol,我国产品称炔睾醇Ia)能抑制垂体前叶腺素的合成或释放,抑制促性腺激素的分泌。为了寻找新的女用避孕药,
The ethynyl hydrogen of 17α-ethynyl androst-5(6)-en-3β, 17β-diol, ethisterone, danazol and their Δ~6 derivatives, and 6-chloro-Δ~6-ethisterone were directly substituted by chlorine when CuCl_2 is used as chlorinating agent and methanol/chloroform as solvent.17α-chloroethynyl-17β-hydroxy derivatives of androst-5(6)-en-3β-ol and androst-4, 6-dien-3-one gave 16-hydroxymethylene-3β-hydroxy-androst-5(6)-en-17-one and 2, 16-dihydroxymethylene androst-4,6-dien-3,17-dione respectively during the hydroxymethylenation, since the elimination of 17α-chloroethynyl group occurred due to the action of sodium methoxide.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1989年第1期31-34,共4页
Journal of China Pharmaceutical University
关键词
达那唑
甾体化合物
消除反应
17α-Chloroethynyl-17β-hydroxy steroid
Copper chloride
Chlorination of ethynyl hydrogen
Elimination